Medicated ointment composition



Patented Aug. 2, E552 UNITED STATES HENRYI. FULLER, OF WASHINGTON, DISTRICT OF COLUMBIA MEDICATED OINTMIENT COMPOSITION No Drawing.

This invention relates to medicated ointment compositions; and in particular it relates to novel compositions of this general class which are characterized by an effective content of a phenylphenol, especially ortho- 1y water-insoluble organic medicaments, of

which one is a phenylphenol, compounded with a suitable ointment base which is of oleaginous nature and generally water-free or substantially so, the medication being tis-' sue-penetrative to a marked degree and therefore effective beyond the seat of application.

It is a well known fact that aqueous solutions of drugs or medicaments which are soluble in water can be mixed with lanoline or other appropriate ointment base, and that when the mixture is applied to the surface of the skin, the medication will be carried into the tissues on account of the ability of the associated water to diffuse. However, where drugs or medicaments contained in ointments as heretofore compounded are insoluble or only difficultly soluble in water, there is usually little or no penetration of the tissues by such medicinal agents, irrespective of whether or not water is present in the mixture, and consequently substantially no remedial action beyond the immediate locus of administration. This is particularly true of the great majority of ointments and salves made with petrolatum, fats, and/or waxes, containing camphor, menthol, eucalyptol, methyl salicylate, thymol, (all of which are grouped for pharmaceutical purposes under the head of volatile oils) salol, or the like, and other preparations of similar character, that are widely used for their reputed value in treating colds, rheumatism, sprains and bruises.

A principal object of the present invention is to improve the character of cerates, ointments, salves, and other mixtures of the general character above discussed, including liquid oleaginous preparations, all of which Application filed February 21, 1930. Serial No. 430,446.

may be generically termed ointment compositions or mixtures, in such manner that penetrative action of water-insoluble or difficultly water-soluble active agents contained in said ointment compositions is brought about or increased without causing irritation of the tissues, thus enhancing the healing, antiseptic, germicidal and/or other desired effects of said agents beyond what has been possible heretofore. Another object is to enable attainment of these results in a relatively simple manner and without unduly increasing the cost of such compositions. Other objects and advantages of the invention will appear as the description proceeds. It has been found that by admixing, with the usual ingredients of ointment compositions which are to include substantially or relatively water-insoluble medicaments. varying percentages of a phenylp'henol (C H .C H OH), particularly orthophenylphenol, compositions are obtainable in which, even though no water has been used in compounding them, the active medicaments will penetrate the tissues when the compositions are applied locally in the usual manner, and will therefore be effective beyond the point of application. The results thus attained are found to be especially pronounced and desirable in the case of organic medicaments, including those specifically named hereinabove as well as others to be mentioned presently. Not only does orthophenylphenol exhibit the peculiar and desirable property of conferring penetrative power upon arelatively Water-insoluble medicament when employed in accordance with the principles of the invention, but it does so without corrosive or other irritating action upon sensitive tissue, even tissue in an already inflamed condition. At the same time it is itself tissue-penetrative and a highly effective antiseptic and germicide also; and it is therefore valuable in a salve whether other medicaments are present or not. Besides being non-irritant and nondestructive of tissue, it is non-toxic in quantities even much exceeding those necessary or desirable to use in ointment compositions.

The metaand para forms of phenylphenol, save that they appear to possess much lower antiseptic and germicidal power, have desirable properties similar to those of orthophenylphenol as ointment composition ingredients and may be employed wholly or partly in lieu thereof where such lower antiseptic and germicidal power is not a deterrent. Ordinarily, however, it is desirable to use the orthocompound, or a mixture of the orthowith either the metaor the paracompound, or both, in which the orthocompound predominates. The orthocompound in particular is commercially available at moderate cost and imparts no disagreeable odor to the mixture, being itself practically odorless.

In their freedom not only from toxicity but also from irritating or corrosive action upon tissues, the phenylphenols are markedly different from phenol (carbolic acid) or the cresols which are. both irritant and toxic in high degree.

In an ointment composition embodying the principles of the invention, the bulk of the composition may consist of any suitable ointment base. In the case of a salve, the base may be an unguent, such as petrolatum, petroleum jelly, a fat such as lanolin or s uet, a fatty acid such as stearic or palmitic, a wax such as beeswax or paraffin wax, or mixtures of one or more of such substances with each other or with an oil capable of softening the unguent used, so that the resulting ointment composition is semi-solid or pasty in consistency. Where a. liquid ointment composition is desired, as in the case of an oil spray preparation for the nose and throat membranes, the ointment base may consist wholly or largely of a bland medicinal oil, such as white mineral oil, for example.

In addition to the base and the phenylphenol, the ointment composition usually contains one or more medicinal agents such as those mentioned hereinabove or others such as oleoresin capsicum, oleoresin ginger, and essential oils like mustard, sassafras, peppermint, rosemary, turpentine, and other therapeutic volatile oils of similar character, which may be used in treating colds, rheumatism, sprains and bruises. These medicaments, while not in and of themselves tissue-penetrant, become so when mixed with phenylphenol, even in small amounts and largely dilutcd with a non-penetratingunguent, such as petrolatum, or with a liquid oil base.

Only a small amount of phenylphenol is required to give effective tissue-penetrating and germicidal properties. While the complete ointment composition may, without harmful results, contain 10% or more of phenylphenol, it is ordinarily suflicient to use smaller amounts, say around 3% to 5%. Even smaller amounts may be employed but ordinarily the amount used should not be much below 2%. Here, as elsewhere in the specification and claims, the stated proportions are by weight.

The amounts of phenylphenol above mentioned are not only sufficient to carry the medicaments of the ointment composition into the tissues effectively but are also sufficient, in the case of orthophenylphenol, to give the desired disinfecting action, even in the absence of other disinfecting substances. Usually the ointment base constitutes over 50%, and more frequently between and 90%, of the complete ointment composition.

The other medicaments commonly used in addition to the phenylphenol, may be present in widely varying proportions relative to each other and to the phenylphenol. Ordinarily their aggregate amount exceeds that of the phenylphenol used and is usually considerably greater, being advantageously from two to six times the amount of the phenylphenol in typical formulae.

In preparing one desirable type of ointment composition embodying the principles of the invention, the following medicaments, including orthophenylphenol, are compounded together in the indicated proportions by weight:

Parts Camphor 3O Eucalyptol 20 Salol v l0 Methyl salicylaten 10 Orthophenylphenol 20 Menthol 5 Thymol 5 This yields a fluid mixture with which a suitable ointment base may be compounded. Thus, for example, if the desired ointment composition is to have a salve-like consistency at ordinary temperatures, 20 parts of the fluid mixture may be added to 80 parts of petrolatum, or to a mixture of 70 to parts of petrolatum with 5 to 10 parts of paraflin. When these ingredients are thoroughly compounded, there results a medicinal salve or ointment which is useful for a variety of purposes, such as treating head and chest colds, muscular aches and pains, sprains, bruises, etc. The medicaments in such an ointment, including especially terpenic volatile oils, and salol, are endowed with marked tissue-penetrating power due to the presence of the orthophe nylphenol; and this type of ointment is regarded as one of the most important and advantageous embodiments of the invention.

The foregoing specific example is to be understood not as restrictive, but as merely illustrative of one advantageous way of compounding ointment compositions in accordance with the broad underlying principles of the invention herein set forth and claimed.

While ointment compositions compounded in accordance with the invention do not require inclusion of water as a constituent and are at least largely, and more often wholly, non-aqueous in character, this does not mean that water must be rigidly excluded in compounding themso long as they retain the characteristics of ointment compositions properly so termed. Likewise reference herein to a substance as substantially or relatively insoluble in water is not to be construed as necessarily signifying complete insolubility in a strict sense. Although the in vention relates more especially to enhancing the tissue-penetrating action of medicaments that are generally classifiable as comparatively insoluble in water, the tissue-penetrating action of Water-soluble medicaments also may be increased by association with a phenyl-phenol in ointment compositions, and the invention in its broader aspects is to be understood as extending thereto.

What is claimed is:

1. An ointment composition comprising an ointment base, with which are compounded a phenylphenol and another medicinal agent.

2. An ointment composition comprising an, ointment base, with which are compounded a phenylphenol and another organic medicinal agent.

3. An ointment composition comprising an ointment base, with which are compounded a phenylphenol and another substantially water-insoluble medicinal agent.

4. An ointment composition comprising an ointment base, with which are compounded a phenylphenol and another substantially water-insoluble organic medicinal agent.

5. An ointment composition as defined in claim 1. wherein the phenylphenol is chiefly ortho henvlphenol.

6. An ointment composition as defined in claim 4, wherein the phenylphenol is chiefly orthophenvlphenol.

7. An ointment composition of salve-like consistency containing a phenylphenol, at least 50 per cent by weight of said composition being an unguent.

8. An ointment composition as defined in claim 7, containing from about2 to 10 per cent of orthophenylphenol.

9. An ointment composition comprising a substantially non-aqueous ointment base. with which are compounded a plurality of relatively water-insoluble meclicaments, one of which is orthophenylphenol employed in minor proportion of the total quantity of said medicaments.

10. An ointment composition comprising an oleaginous base,with which are compounded a therapeutic volatile oil and a phenylphenol.

11. An ointment composition comprising an oleaginous base, with which are compounded a plurality of therapeutic volatile oils, including a terpenic oil, and orthophenylphenol.

12. An ointment composition comprising an oleaginous base, with which are compounded salol, a therapeutic volatile oil, and orthophenylphenol.

13. An ointment composition comprising 'petrolatum with which are compounded cam- In testimony whereof I hereunto aflix my signature.

HENRY O. FULLER. 

